In vitro lipolysis models as a tool for the characterization of oral lilpid and surfactant based drug delivery systems

TY - JOUR

T1 - In vitro lipolysis models as a tool for the characterization of oral lilpid and surfactant based drug delivery systems

AU - Larsen, Anne Tungelund

AU - Sassene, Philip

AU - Müllertz, Anette

PY - 2011/9/30

Y1 - 2011/9/30

N2 - With the increasing interest in lipid and surfactant based drug delivery systems (LSBDDS) for oral delivery of poorly soluble drugs, the need for efficient development tools is emerging. In vitro lipolysis models, simulating the digestion in the small intestine, is a promising tool in this regard. Several different in vitro lipolysis models have been used for characterization of LSBDDS, all using porcine pancreatin as lipase source, and primarily differing in the addition scheme of calcium and the kind of bile acids employed. Both calcium and bile influence the lipolysis. Calcium have been used both as fixed addition at the beginning of the experiment and with a continuous addition during lipolysis. Both pure bile acids and crude porcine bile extract have been used. Lipolysis of LSBDDS will generate mixed micelles, as well as lamellar and hexagonal phases. These have been characterized by dynamic light scattering, cryogenic transmission electron microscopy and small angle X-ray scattering. The faith of drug during in vitro digestion of a LSBDDS is often studied by ultracentrifugation and quantification of drug in the different phases formed. Further, drug precipitated during in vitro lipolysis has been characterized by X-ray powder diffraction and polarized light microscopy.

AB - With the increasing interest in lipid and surfactant based drug delivery systems (LSBDDS) for oral delivery of poorly soluble drugs, the need for efficient development tools is emerging. In vitro lipolysis models, simulating the digestion in the small intestine, is a promising tool in this regard. Several different in vitro lipolysis models have been used for characterization of LSBDDS, all using porcine pancreatin as lipase source, and primarily differing in the addition scheme of calcium and the kind of bile acids employed. Both calcium and bile influence the lipolysis. Calcium have been used both as fixed addition at the beginning of the experiment and with a continuous addition during lipolysis. Both pure bile acids and crude porcine bile extract have been used. Lipolysis of LSBDDS will generate mixed micelles, as well as lamellar and hexagonal phases. These have been characterized by dynamic light scattering, cryogenic transmission electron microscopy and small angle X-ray scattering. The faith of drug during in vitro digestion of a LSBDDS is often studied by ultracentrifugation and quantification of drug in the different phases formed. Further, drug precipitated during in vitro lipolysis has been characterized by X-ray powder diffraction and polarized light microscopy.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1016/j.ijpharm.2011.03.002

DO - 10.1016/j.ijpharm.2011.03.002

M3 - Journal article

SN - 0378-5173

VL - 417

SP - 245

EP - 255

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -